Acetylcholine (ACh) is a kind of neurotransmitter released from the cholinergic nerve ending including motor nerve fiber, vegetative nerve preganglionic fiber, parasympathetic postganglionic fiber and part of sympathetic postganglionic fiber, which acts on cholinergic receptors, i.e., muscarine receptor (M-receptor) and nicotine receptor (N-receptor), with strong bioactivity. Cholinergic receptor blocking agents, which can be divided into M-choline receptor blocking agents and N-choline receptor blocking agents, act to block the choline receptor. M-choline receptor blocking agents can block the choline receptors on the effectors dominated by the central and the postganglionic cholinergic nerve, which exhibits pseudo-mentation of the central nerve, chalasia of the smooth muscles, inhibition of glandular secretion, mydriasis, speeded cardiac rhythm and the like, and thus, they have extensive pharmacological functions and clinical uses.
At present, nearly all of M-choline receptor blocking agents are tropine-base alkaloids or artificial atropine substitutes. Due to their extensive pharmacological effects, when they are used for a certain effect, other effects become side effects, especially the psychomimetic effect. This limits their clinical uses and thus, the anticholinergic agents should have selectivity, i.e., maintaining their anticholinergic effect while reducing the adverse effect of the center nerve psychomimetic effect.
Up to this date, there is no report about the quinuclidine compounds having a quaternary ammonium group as disclosed in the present invention, nor is there any report about the use thereof in blocking cholinergic receptor as an anticholinergic agent.